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Polymeric curcumin nanoparticles by a facile in situ method for macrophage targeted delivery

机译:高分子姜黄素纳米粒子通过方便的原位方法用于巨噬细胞靶向输送

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摘要

Targeting macrophages is a promising strategy for improved therapy of intracellular infections as macrophages exhibit rapid phagocytosis of particles >200 nm. Entrapment of Curcumin (CUR) in nanocarriers could provide bioenhancement and macrophage targeting. We present a simple and facile in situ nanoprecipitation approach for instantaneous and on‐site generation of curcumin nanoparticles (ISCurNP). ISCurNP optimised by Box‐Behnken design exhibited average size of 208.25 ± 7.55 nm and entrapment efficiency of 90.16 ± 1.17%. Differential scanning calorimetry and X‐Ray diffraction confirmed amorphization of CUR in ISCurNP. Sustained release was observed over 72 hr in vitro at lysosomal pH 4.5. Rapid and high uptake in RAW 264.7 macrophages was confirmed by flow cytometry and high performance liquid chromatography. Confocal microscopy established localisation of ISCurNP in lysosomal compartment. The facile in situ nanoprecipitation method provides simple, scalable technology to enable macrophage targeted delivery of CUR, with great promise for improved therapy of intracellular infections.
机译:靶向巨噬细胞是改善细胞内感染治疗的一种有前途的策略,因为巨噬细胞显示了> 200 nm的颗粒的快速吞噬作用。姜黄素(CUR)截留在纳米载体中可以提供生物增强和巨噬细胞靶向。我们为姜黄素纳米粒子(ISCurNP)的即时和现场生成提供了一种简单而便捷的原位纳米沉淀方法。通过Box-Behnken设计优化的ISCurNP的平均粒径为208.25±7.55 nm,包封效率为90.16±1.17%。差示扫描量热法和X射线衍射证实了ISCurNP中CUR的非晶化。在溶酶体pH 4.5下,在体外72小时内观察到缓释。流式细胞仪和高效液相色谱法证实了RAW 264.7巨噬细胞的快速摄取。共聚焦显微镜确定了ISCurNP在溶酶体区室中的定位。简便的原位纳米沉淀方法提供了简单,可扩展的技术,以使巨噬细胞靶向递送CUR,并有望改善细胞内感染的治疗方法。

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